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本文报道用薄层-荧光扫描法,研究阿克拉霉素 A(ACMA)在正常大鼠及荷瘤小鼠体内吸收、分布及排泄的结果。经静脉注射给药后,ACMA的血药浓度迅速下降,其分布相(T_1/2α)为4.8分钟,消除相(T_1/2β)为10.22小时。ACMA及其糖苷类(GM)代谢物的分布以肺为最高,其次为脾、胸腺和小肠,肿瘤组织中有一定量的ACMA及糖苷类代谢物。配基型(AM)代谢物则以肝脏为最高。ACMA本身自尿和粪便中排出量很少,给药后 30小时,即不能在尿中检出ACMA,只可检出GM型及AM型代谢物。粪便中主要为配基型(AM)代谢物。给药后ACMA自胆汁排泄率为7％。GM型代谢物为8％,AM型为2％。
This paper reports the use of TLC-fluorescence scanning method to study the absorption, distribution and excretion of aclacinomycin A (ACMA) in normal and tumor-bearing mice. After intravenous injection, the plasma concentration of ACMA decreased rapidly with a distribution phase (T 1 / 2α) of 4.8 minutes and elimination phase (T 1 / 2β) of 10.22 hours. The distribution of ACMA and its metabolites was the highest in the lungs, followed by the spleen, thymus and small intestine. There was a certain amount of ACMA and glycoside metabolites in the tumor tissue. With base type (AM) metabolites in the liver is the highest. ACMA itself excretes very little from the urine and excrement, 30 hours after administration, that is, ACMA can not be detected in the urine, and only GM-type and AM-type metabolites can be detected. The droppings are predominantly ligand-based (AM) metabolites. After administration of ACMA from bile excretion rate of 7%. GM type metabolites 8%, AM type 2%.